AU2015369983C1 - Thieno[2,3-c]pyrrol-4-one derivatives as ERK inhibitors - Google Patents

Thieno[2,3-c]pyrrol-4-one derivatives as ERK inhibitors Download PDF

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Publication number
AU2015369983C1
AU2015369983C1 AU2015369983A AU2015369983A AU2015369983C1 AU 2015369983 C1 AU2015369983 C1 AU 2015369983C1 AU 2015369983 A AU2015369983 A AU 2015369983A AU 2015369983 A AU2015369983 A AU 2015369983A AU 2015369983 C1 AU2015369983 C1 AU 2015369983C1
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compound
cancer
mmol
pyrrol
methyl
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AU2015369983A1 (en
AU2015369983B2 (en
Inventor
Guillermo S. Cortez
Sajan Joseph
Johnathan Alexander Mclean
William T. Mcmillen
Michael John Rodriguez
Gaiying ZHAO
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Eli Lilly and Co
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Eli Lilly and Co
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Publication of AU2015369983C1 publication Critical patent/AU2015369983C1/en
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00Medicinal preparations containing antigens or antibodies
    • A61K39/395Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/08Bridged systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2863Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against receptors for growth factors, growth regulators

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Endocrinology (AREA)
  • Mycology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
AU2015369983A 2014-12-22 2015-12-16 Thieno[2,3-c]pyrrol-4-one derivatives as ERK inhibitors Ceased AU2015369983C1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462095185P 2014-12-22 2014-12-22
US62/095,185 2014-12-22
PCT/US2015/065940 WO2016106029A1 (en) 2014-12-22 2015-12-16 Thieno[2,3-c]pyrrol-4-one derivatives as erk inhibitors

Publications (3)

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AU2015369983A1 AU2015369983A1 (en) 2017-05-25
AU2015369983B2 AU2015369983B2 (en) 2018-08-23
AU2015369983C1 true AU2015369983C1 (en) 2019-02-21

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AU2015369983A Ceased AU2015369983C1 (en) 2014-12-22 2015-12-16 Thieno[2,3-c]pyrrol-4-one derivatives as ERK inhibitors

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US (3) US9469652B2 (de)
EP (1) EP3237423B1 (de)
JP (1) JP6445701B2 (de)
KR (1) KR101917972B1 (de)
CN (1) CN107108648B (de)
AR (1) AR102977A1 (de)
AU (1) AU2015369983C1 (de)
BR (1) BR112017011130A2 (de)
CA (1) CA2966559C (de)
CL (1) CL2017001514A1 (de)
CO (1) CO2017005217A2 (de)
CR (1) CR20170182A (de)
CY (1) CY1121831T1 (de)
DK (1) DK3237423T3 (de)
DO (1) DOP2017000122A (de)
EA (1) EA031659B1 (de)
EC (1) ECSP17038500A (de)
ES (1) ES2738406T3 (de)
GT (1) GT201700134A (de)
HR (1) HRP20191268T1 (de)
HU (1) HUE045933T2 (de)
IL (1) IL252065B (de)
JO (1) JO3596B1 (de)
LT (1) LT3237423T (de)
MA (1) MA41251B1 (de)
MD (1) MD3237423T2 (de)
ME (1) ME03490B (de)
MX (1) MX371206B (de)
MY (1) MY178426A (de)
NZ (1) NZ731531A (de)
PE (1) PE20171043A1 (de)
PH (1) PH12017501155B1 (de)
PL (1) PL3237423T3 (de)
PT (1) PT3237423T (de)
RS (1) RS59015B1 (de)
SG (1) SG11201704521SA (de)
SI (1) SI3237423T1 (de)
SV (1) SV2017005443A (de)
TN (1) TN2017000233A1 (de)
TR (1) TR201909887T4 (de)
TW (1) TWI704151B (de)
UA (1) UA119686C2 (de)
WO (1) WO2016106029A1 (de)
ZA (1) ZA201702786B (de)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201602572YA (en) 2013-10-03 2016-04-28 Kura Oncology Inc Inhibitors of erk and methods of use
TWI704151B (zh) * 2014-12-22 2020-09-11 美商美國禮來大藥廠 Erk抑制劑
ES2700200T3 (es) 2014-12-22 2019-02-14 Lilly Co Eli Inhibidores de ERK
EP3365334B1 (de) 2015-10-21 2024-07-17 Otsuka Pharmaceutical Co., Ltd. Benzolactam-verbindungen als proteinkinasehemmer
JP2019523778A (ja) * 2016-06-29 2019-08-29 イーライ リリー アンド カンパニー 膵癌の治療に使用するための、erk1/2阻害剤化合物と、ゲムシタビン、またはゲムシタビンおよびnab−パクリタキセルとの併用
WO2018081204A1 (en) * 2016-10-26 2018-05-03 Li George Y DEUTERATED N-(5-((4-ETHYLPIPERAZIN-1-YL)METHYL) PYRIDIN-2-YL)-5-FLUORO-4-(4-FLUORO-1-ISOPROPYL-2-METHYL-1H-BENZO[d]IMIDAZOL-6-YL)PYRIMIDIN-2-AMINE
GB201706327D0 (en) 2017-04-20 2017-06-07 Otsuka Pharma Co Ltd A pharmaceutical compound
JP7312171B2 (ja) 2017-11-24 2023-07-20 ヤンセン ファーマシューティカ エヌ.ベー. ピラゾロピリジノン化合物
AU2019253706A1 (en) * 2018-04-09 2020-11-26 G1 Therapeutics, Inc. Treatment of cancers having driving oncogenic mutations
CA3101117A1 (en) * 2018-05-22 2019-11-28 Js Innomed Holdings Ltd. Heterocyclic compounds as kinase inhibitors, compositions comprising the heterocyclic compound, and methods of use thereof
US20220040324A1 (en) 2018-12-21 2022-02-10 Daiichi Sankyo Company, Limited Combination of antibody-drug conjugate and kinase inhibitor
EP3946620B1 (de) * 2019-03-27 2023-04-26 Eli Lilly and Company Salze der 5,6-dihydro-4h-thieno[2,3-c]pyrrol-4-on-verbindung als erk-inhibitoren
BR112021017957A2 (pt) * 2019-03-28 2021-11-23 Jiangsu Hengrui Medicine Co Derivado tienoeterocíclico, método de preparação do mesmo e uso médico do mesmo
CA3135070A1 (en) * 2019-03-29 2020-10-08 Jiangsu Hengrui Medicine Co., Ltd. Pyrroloheterocyclic derivative, preparation method therefor, and application thereof in medicine
US20220168250A1 (en) * 2019-05-16 2022-06-02 Eli Lilly And Company TRIPLE COMBINATION OF AN ERK1/2 INHIBITOR WITH A BRAF INHIBITOR AND AN EGFR INHIBITOR FOR USE IN THE TREATMENT OF BRAFv6ooE COLORECTAL CANCER
CN112457326B (zh) * 2019-09-06 2022-02-15 上海凌达生物医药有限公司 一类芳香杂环并内酰胺类化合物、制备方法和用途
TWI765451B (zh) * 2019-12-06 2022-05-21 大陸商南京明德新藥研發有限公司 作為erk抑制劑的螺環類化合物及其應用
CN110950876B (zh) * 2019-12-10 2021-08-17 上海凌达生物医药有限公司 一类呋喃并内酰胺类化合物、制备方法和用途
WO2021216777A1 (en) * 2020-04-21 2021-10-28 The Trustees Of The Stevens Institute Of Technology Erk inhibitors for cancer therapy
CN114315837B (zh) * 2020-09-29 2023-06-16 江苏恒瑞医药股份有限公司 一种erk抑制剂的结晶形式及其制备方法
WO2022068860A1 (zh) * 2020-09-29 2022-04-07 江苏恒瑞医药股份有限公司 一种吡咯并杂环类衍生物的晶型及其制备方法
TWI825811B (zh) * 2021-06-28 2023-12-11 大陸商德昇濟醫藥(無錫)有限公司 噻唑並內醯胺並螺雜環類化合物及其應用
WO2023087027A1 (en) * 2021-11-15 2023-05-19 Erasca, Inc. Thiophene ulk1/2 inhibitors and their use thereof
WO2023137297A2 (en) * 2022-01-11 2023-07-20 Suvalent Therapeutics, Inc. 5,6-dihydro-4h-thieno[2,3-c]pyrrole sumo inhibitors and uses thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030064982A1 (en) * 2000-09-15 2003-04-03 Robert Davies Pyrazole compounds useful as protein kinase inhibitors
WO2007053776A1 (en) * 2005-11-03 2007-05-10 Sgx Pharmaceuticals, Inc. Pyrimidinyl-thiophene kinase modulators
WO2010075074A1 (en) * 2008-12-22 2010-07-01 Eli Lilly And Company Protein kinase inhibitors
WO2013130976A1 (en) * 2012-03-01 2013-09-06 Array Biopharma Inc. Serine/threonine kinase inhibitors

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4023048A1 (de) * 1990-07-20 1992-01-23 Basf Ag Dicarbonsaeureimide, verfahren zu ihrer herstellung und ihre verwendung als herbizide
JP4105948B2 (ja) * 2000-09-15 2008-06-25 バーテックス ファーマシューティカルズ インコーポレイテッド プロテインキナーゼインヒビターとして有用なピラゾール化合物
JP2005526506A (ja) 2002-03-04 2005-09-08 イムクローン システムズ インコーポレイティド Kdrに特異的なヒト抗体及びその利用
JP4688498B2 (ja) * 2002-11-04 2011-05-25 バーテックス ファーマシューティカルズ インコーポレイテッド Jakインヒビターとしてのヘテロアリール−ピリミジン誘導体
UA80571C2 (en) 2002-11-22 2007-10-10 Lilly Co Eli Quinolinyl-pyrrolopyrazoles
EP2326627A1 (de) 2008-08-20 2011-06-01 Schering Corporation Substituierte pyridin- und pyrimidinderivate und ihre verwendung bei der behandlung von virusinfektionen
EP2346860B1 (de) * 2008-10-08 2012-09-19 Bristol-Myers Squibb Company Pyrrolone als antagonisten des rezeptoreptors 1 für das melanin konzentrierende hormon
BR112013007499A2 (pt) * 2010-09-01 2016-07-12 Genentech Inc piridazinonas - métodos de criação e usos
JO3148B1 (ar) 2011-07-27 2017-09-20 Lilly Co Eli مركب مثبط لإشارات مسار notch
AR090151A1 (es) 2012-03-07 2014-10-22 Lilly Co Eli Compuestos inhibidores de raf
CA2883807A1 (en) * 2012-09-28 2014-04-03 Boehringer Ingelheim International Gmbh Pharmaceutical combinations comprising dual angiopoietin-2 / dll4 binders and anti-vegf-r agents
ES2700200T3 (es) * 2014-12-22 2019-02-14 Lilly Co Eli Inhibidores de ERK
TWI704151B (zh) * 2014-12-22 2020-09-11 美商美國禮來大藥廠 Erk抑制劑

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20030064982A1 (en) * 2000-09-15 2003-04-03 Robert Davies Pyrazole compounds useful as protein kinase inhibitors
WO2007053776A1 (en) * 2005-11-03 2007-05-10 Sgx Pharmaceuticals, Inc. Pyrimidinyl-thiophene kinase modulators
WO2010075074A1 (en) * 2008-12-22 2010-07-01 Eli Lilly And Company Protein kinase inhibitors
WO2013130976A1 (en) * 2012-03-01 2013-09-06 Array Biopharma Inc. Serine/threonine kinase inhibitors

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
SPRATLIN, J., 'Ramucirumab (IMC-1121B): Monoclonal Antibody Inhibition of Vascular Endothelial Growth Factor Receptor-2', Current Oncology Reports, 2011, Vol. 13(2), pages 97-102. *

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Publication number Publication date
PT3237423T (pt) 2019-08-21
SI3237423T1 (sl) 2019-08-30
US20160375030A1 (en) 2016-12-29
KR20170083145A (ko) 2017-07-17
DK3237423T3 (da) 2019-07-22
TW201632530A (zh) 2016-09-16
IL252065A0 (en) 2017-07-31
MY178426A (en) 2020-10-13
KR101917972B1 (ko) 2018-11-12
ZA201702786B (en) 2019-02-27
ES2738406T3 (es) 2020-01-22
USRE48635E1 (en) 2021-07-13
JP6445701B2 (ja) 2018-12-26
HUE045933T2 (hu) 2020-01-28
SV2017005443A (es) 2018-08-27
US9469652B2 (en) 2016-10-18
PE20171043A1 (es) 2017-07-19
CR20170182A (es) 2017-06-21
JO3596B1 (ar) 2020-07-05
NZ731531A (en) 2018-12-21
DOP2017000122A (es) 2017-06-15
TWI704151B (zh) 2020-09-11
ME03490B (de) 2020-01-20
CN107108648A (zh) 2017-08-29
TR201909887T4 (tr) 2019-07-22
UA119686C2 (uk) 2019-07-25
CY1121831T1 (el) 2020-07-31
GT201700134A (es) 2018-11-23
EA201791133A1 (ru) 2017-10-31
AU2015369983A1 (en) 2017-05-25
ECSP17038500A (es) 2017-12-01
JP2017538768A (ja) 2017-12-28
PH12017501155A1 (en) 2017-11-27
US9526733B1 (en) 2016-12-27
CA2966559C (en) 2019-06-18
BR112017011130A2 (pt) 2017-12-26
CO2017005217A2 (es) 2017-09-20
HRP20191268T1 (hr) 2019-11-01
EA031659B1 (ru) 2019-02-28
RS59015B1 (sr) 2019-08-30
PH12017501155B1 (en) 2017-11-27
IL252065B (en) 2020-08-31
US20160176896A1 (en) 2016-06-23
AU2015369983B2 (en) 2018-08-23
CL2017001514A1 (es) 2018-02-09
AR102977A1 (es) 2017-04-05
MX371206B (es) 2020-01-22
MD3237423T2 (ro) 2019-11-30
MA41251A (fr) 2017-11-01
PL3237423T3 (pl) 2020-01-31
EP3237423A1 (de) 2017-11-01
MA41251B1 (fr) 2019-09-30
MX2017008242A (es) 2017-10-06
LT3237423T (lt) 2019-08-26
EP3237423B1 (de) 2019-06-05
CN107108648B (zh) 2019-07-12
TN2017000233A1 (en) 2018-10-19
WO2016106029A1 (en) 2016-06-30
SG11201704521SA (en) 2017-07-28
CA2966559A1 (en) 2016-06-30

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